Chemical Constituents and Biological Importance of Swertia: A Review
Jagmohan S. Negi,
Swertia, commonly known as Chirata in indigenous systems of medicine, are used for treatment of a variety of ailments. Literature survey revealed that much phytochemical analysis has been done on genus Swertia by several groups. In this study, we had planned to document the active chemical constituents of valuable medicinal plants of genus Swertia. The major bioactives of Swertia are xanthones, however, other secondary metabolites such as flavonoids, iridoid glycosides and triterpenoids are also active constituents of this genus. These secondary metabolites played significant role in biological activities such as hepatoprotective, antihepatotoxic, antimicrobial, anti-inflammatory, anticarcinogenic, antileprosy, hypoglycemic, antimalarial, antioxidant, anticholinergic, CNS depressant and mutagenicity.
Received: October 22, 2010;
Accepted: February 19, 2011;
Published: April 22, 2011
Swertia (family Gentianaceae) is a large genus of herbs distributed in the
mountainous regions of tropical area at an altitude of 1200-3600 m. The herbal
drug chiretta obtained from the dried plants of swertia species.
The whole plants of Swertia are medicinal but roots are the most powerful parts
(Anonymous, 1976). These are useful as a tonic without
aroma or astringency. In Indian medical system chiretta is used as remedy for
bronchial asthma, liver disorders, chronic fever, anemia, stomachic and diarrhoea.
Chiretta is also used in dying cotton cloth and in liquor industry as bitter
ingredients. In Ayurveda, S. chirayita is used as antipyretic, anthelminitic,
antiperiodic, laxative and in asthma and leucorrhoea. In Yunani system the plant
is used as astringent, tonic, stomachic, lessens inflammation, sedative to pregnant
uterus and chronic fevers (Kirtikar and Basu, 1984).
S. chirayita has an established domestic (India) and international market
which is increasing at a rate of 10% annually. In spite of the increasing demand
by herbal industry the plant is still collected from wild. It is sparsely cultivated
and negligible efforts have gone into developing proper agro-techniques of plant.
It is harvested for the drug industry (Bentley and Trimen,
1880). S. chirayita is also used in British and American pharmacopoeias
as tincture and infusions (Joshi and Dhawan, 2005).
S. angustifolia resembles to S. chirayita very closely but differs
from it in having thinner root, small wings and ridges on the stem. The dried
plants of S. angustifolia and S. paniculata are used as substitute
for S. chirayita. About 22,000 kg of the drug are said to be collected
and sold annually in Himanchal Pradesh while the annual demand for chiretta
in India is reported to be 37,300 kg. Plants belonging to these families are
found in all parts of world. They have been widely used in folk medicine. Simple
polyoxygenated xanthones have been isolated from most of them. Xanthone derivatives,
flavonoids, iridoid glycosides, triterpenoids and dimeric xanthones have been
isolated from the genus Swertia (Tan et al., 1991;
Zhou et al., 1989). The genus Swertia exhibit
variety of biological activity such as hepatoprotective, antihepatotoxic, antimicrobial,
anti-inflammatory, anticarcinogenic, antileprosy, hypoglycemic, antimalarial,
antioxidant, anticholinergic, CNS depressant and mutagenicity. The pharmacological
properties of Swertia have raised great interest. The purpose of this review
to collect all the possible information regarding the chemical constituents
and biological effects of the genus Swertia, thus will help to the researchers
and scientists to take action for future study in this discipline.
Xanthones are main secondary metabolites of Swertia species. Structures of
xanthones are related to that of flavonoids and their chromatographic behaviors
are also similar. Although flavonoids are frequently encountered in nature,
xanthones have been found in limited number of families. They always occur in
Gentianaceae and Guttiferae. Xanthones are sometimes found as the parent polyhydroxylated
compounds but most xanthones are mono or poly methyl ethers or are found as
glycosides (Hostettmann and Miura, 1977). Unlike iridoids,
xanthones are apparently not present in all plant species investigated in the
family Gentianaceae. This is documented by the systematic study of Hostettmann-Kaldas
et al. (1981). The natural xanthones have been isolated mainly from
about 150 plants associated with four families; Guttiferae, Gentianaceae, Moraceae
and Polygalaceae. According to Vieira and Kijjoa (2005),
278 natural xanthones were reported from total of 515 xanthones. In this period,
the xanthones from higher plants appear to be associated mainly with the families
Clusiaceae (55 species in 12 genera) and Gentianaceae (28 species in 8 genera).
Isolated compounds and biological activities of Swertia species are listed in
Table 1. Xanthones isolated from nature are classified into
six main groups; simple xanthones, xanthone glycosides, prenylated xanthones,
xanthonolignoids, bis-xanthones and miscellaneous xanthones. These are further
subdivided according to the degree of oxygenation into non-, mon-o, di-, tri-,
tetra-, penta- and hexa-oxygenated substances (Mandal et
al., 1992b; Sultanbawa, 1980; Demirkiran,
Xanthones and their glycosides (Fig. 1) have been isolated
from Swertia species. Mangiferin is the most common C-glycosides in S. chirayita,
S. mussotii, S. cordata, S. macrosperma and S. connata.
Xanthone O-glycosides (swertianolin) from S. japonica and S. ciliata
(Plouvier et al., 1967) have been reported. The
first xanthone O-glycoside, norswertianin-1-O-glucosyl-3-O-glucoside has been
isolated from S. perennis (Hostettmann and Wagner,
1977). The isolated chemical constituents, ethno-pharmacology as well as
the biological activities and pharmacological applications of Swertia species,
covering the literature up to 2003 are compiled by Brahmachari
et al. (2004). Xanthones in Swertia chirata, S. speciosa and
S. paniculata were determined by HPLC (Negi et al.,
2009a, 2010a, b). Mineral
elements, based on their concentration can play different roles in human health
and plant life. Nine elements (Zn, Cu, Mn, Fe, Co Na, K, Ca and Li) in S.
chirayita and S. speciosa have been analyzed by atomic absorption
spectrometry (Negi et al., 2009b, 2010c).
Kaempferol, catechin, epicatechin and Polyphenol Contents were also isolated
and identified from Swietenia macrophylla, Rhus coriaria and Rhus
typhina (Falah et al., 2008; Kossah
et al., 2010). Extracts of G. senegalensis are rich in flavonoid
content and showed anti-inflammatory activity (Sombie et
al., 2011). Leaf and stem of Swertia chirata showed significant
antimicrobial activities against some Gram-positive and Gram-negative bacteria
(Alam et al., 2009).
|| Isolated compounds and activity of different parts of Swertia
Several isolated chemical constituents viz, coumarins, flavonoids, phytosterol,
phenols, tenins, alkaloids, triterpenes, anthraquinons and biological activities
of Toona species were documented by Negi et al. (2011).
|| Structures of some isolated xanthones from Swertia
Plants belonging to the family Gentianaceae, are best known for their bitter
taste and used in traditional remedies against loss of appetite, fever and are
still included in many tonic formulations (Gaur,
1999). Some specific activities have been reported for xanthones and iridoids
from Gentianaceae. Iridoids such as swertiamarin have anticholinergic propertiy
(Bhattacharya et al., 1974). For sweroside and
gentiopicroside hepatoprotective activities have been reported (Kondo
et al., 1994) and both compounds are being used as antihepatitis
drugs. Xanthones (especially mangiferin) are reported to give CNS stimulation
(Bhattacharya et al., 1972). They should also
have anti-inflammatory activity (Mandal et al., 1992a).
For bellidifolin and swerchirin a strong hypoglycemic activity has been reported
by Saxena et al. (1993) and Basnet et al.
(1994). S. paniculata is used in the Indian System of Medicine as a bitter
tonic and in the treatment of some mental disorders (Prakash
et al., 1982). S. hookeri extract is used in the treatment
of microbial infections and as a mood elevator (Ghosal et
al., 1980). Swertifrancheside isolated from S. franchetiana was
found to be potent inhibitor of the DNA polymerase activity of human immunodeficiency
virus-1 reverse transcriptase (HIV-1RT). Naturally occurring xanthones have
emerged out as an important class of organic compounds in view of their remarkable
pharmacological and other biological activities. It has now been observed that
a number of plant products which are in regular use as chemotherapeutic agents
contain xanthones as active constituents. Mangiferin was the first xanthone
to be investigated pharmacologically and has been found to exhibit a broad spectrum
of biological activities. It shows monoamine oxidase inhibition, cardiotonic,
convulsant and choleretic activities (Ghosal et al.,
1973; Bhattacharya et al., 1972). Pronounced
anti-inflammatory activity has also been observed in mangiferin. Oral and topical
compounds containing mangiferin are useful for the treatment of diseases caused
by herpes virus. Mangiferin has been found to protect the liver of the rats
from high altitude hypoxia. On the other hand Ghosal
et al. (1975) have observed the opposite CNS depressant effect for xanthone-O-glycosides
in mice and rats. The extract of most of Swertia species showed mutagenic activities.
The antimalarial drug AYUSH-64 contains S. chirayita as one of the ingredients.
Xanthones of S. chirayita are reported to produce CNS depression (Ghosal
et al., 1973). The total extract of S. chirayita showed significant
antifeedant activity against Jute semilooper (Malic
et al., 1985). Norswertianolin, an O-glycoside has been reported
to produce antitubercular activity. The O-glycosides of S. purpurescens
are known to produce CNS depression in albino rate and mice (Ghosal
et al., 1974). 1,8-Dihydroxy-3,5-dimethoxyxanthone (swerchirin),
isolated from the hexane fraction of Swertia chirayita, has a very significant
blood sugar lowering effect in fasted, fed, glucose loaded and tolbutamide pre-treated
As a conclusion, the present study has shown that mainly xanthones from genus Swertia are responsible for several types of biological activities. Apart from these flavonoids, iridoid glycosides and triterpenoids are also secondary metabolites isolated from this genus which also contribute their role in biological activities.
The authors are thankful to Dr. Asha Budakoti, NCL, Pune for providing some references.
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